Amphiphilic chitosan derivative drug-loaded nano-micelle and preparation method

A technology of chitosan derivatives and amphiphilic polymers is applied in the field of pharmaceutical preparations, which can solve the problems of poor pharmacokinetic properties, prevent drug absorption, and difficult to absorb, and achieve prolonging blood circulation time and bioadhesion. Promoting, good biocompatibility effect

Inactive Publication Date: 2016-06-22
BEIJING UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] (1) Low solubility, most drugs are hydrophobic, poorly soluble in aqueous solution, easy to precipitate, need to add solubilizer, co-solvent or latent solvent to improve solubility;
[0006] (2) Toxic and side effects are large, and the distribution selectivity in the body after administration is poor
In addition, the addition of excipients is likely to cause serious side effects, such as allergic reactions after administration, toxic kidney damage, neurotoxicity, bone marrow suppression, etc., which seriously af

Method used

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  • Amphiphilic chitosan derivative drug-loaded nano-micelle and preparation method
  • Amphiphilic chitosan derivative drug-loaded nano-micelle and preparation method
  • Amphiphilic chitosan derivative drug-loaded nano-micelle and preparation method

Examples

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[0032] Example 1

[0033] (1) Prepare blank amphiphilic polymer micelles: dissolve 5 mg of amphiphilic polymer chitosan-vitamin E succinate-N-acetyl-L-cysteine ​​in 5 ml of deionized water, and magnetically stir Until it is completely dissolved and mixed evenly, pass the obtained polymer solution through a medium-speed filter paper with a pore size of 30-50 μm, and then through a 0.8 μm filter membrane, centrifuge at 4000 r / min for 5 minutes, and take the supernatant through a 0.45 μm needle filter The first two drops were discarded, and the final solution was sonicated for 10 minutes under a probe-type ultrasonic instrument (power 150W, working 5s, intermittent 3s). The obtained solution was centrifuged at 3000 r / min for 5 min, and the supernatant was passed through a 0.45 μm needle filter membrane to obtain blank amphiphilic polymer micelles.

[0034] (2) Amphiphilic polymer drug-loaded nanomicelles

[0035] Add 5 mg of amphiphilic polymer chitosan-vitamin E succinate-N-acet...

Example Embodiment

[0045] Example 2

[0046] Add 5 mg of amphiphilic polymer chitosan-vitamin E succinate-N-acetyl-L-cysteine ​​to 5 ml of deionized water, stir magnetically until completely dissolved and mix evenly, and the resulting polymer solution is first Pass through a medium-speed filter paper with a pore size of 30-50 μm, and then pass through a 0.8 μm filter membrane, centrifuge at 4000 r / min for 5 minutes, take the supernatant and pass it through a 0.45 μm needle filter, discard the first two drops, and obtain the amphiphilic polymer solution. Dissolve 5 mg of camptothecin that has been weighed in the corresponding solvent, and stir magnetically to make the camptothecin dissolve evenly. When the polymer solution is stirred, the dissolved camptothecin solution is added dropwise to the amphiphilic polymer solution, and the above two mixed solutions that have been stirred are evaporated out of the solvent using a rotary evaporator under reduced pressure, and start Stop when turbidity ap...

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Abstract

The invention discloses an amphiphilic chitosan derivative drug-loaded nano-micelle and a preparation method and belongs to the field of pharmaceutical preparations. Amphiphilic chitosan derivatives form the micelle by means of self assembling, vitamin E succinate serves as a kernel, and thiolated chitosan serves as a shell; the hydrophobic kernel is used for entrapping a hydrophobic anti-HIV drug, the shell carrying positive charges is used for adsorbing cytomembrane, the loaded drug can be stably released in vivo, the hydrophilic shell is used for enhancing the solubility of the micelle and maintaining the stability of the micelle in a solution, and then the blood circulation time of the micelle after systematic administration is prolonged. The micelle can stably exist in all kinds of body fluid for more than 10 hours after particles are formed, the particle size is smaller than 200 nanometers, and it is beneficial for controlling the micelle particles to enter cells without being removed by macrophages. The delivery system can keep stability under the condition that serums exist, the drug is delivered into the cells, and good biocompatibility is achieved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an amphiphilic chitosan derivative (chitosan-vitamin E succinate-N-acetyl-L-cysteine) nano-micelle, a preparation method and an application thereof. Background technique [0002] With the deterioration of the global ecological environment and the increasing pace of people's life and work pressure, the morbidity and mortality of AIDS, a major disease that seriously threatens human life and health, are increasing year by year. China is the largest country in Asia, and its economy has developed rapidly in recent years, but at the same time, AIDS is also quietly attacking this country. Now China has become one of the fastest-growing countries in the world for AIDS. [0003] By the end of 2009, it was estimated that there were about 740,000 people living with HIV / AIDS in China, including 105,000 AIDS patients; it was estimated that there were 48,000 new HIV infections and 26,...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/36A61K31/506A61K31/4745A61P31/18
CPCA61K9/1075A61K31/4745A61K31/506A61K47/36
Inventor 胡利明吴加周曾程初王小利
Owner BEIJING UNIV OF TECH
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